标题:Developments of DNA-dependent Protein Kinase Inhibitors as Anticancer Agents
作者:Ma, Chen-Chen;Li, Hui;Wan, Ren-Zhong;Liu, Zhao-Peng
作者机构:[Ma, C.-C] Institute of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong U 更多
通讯作者:Liu, ZP
通讯作者地址:[Liu, ZP]Shandong Univ, Inst Med Chem, Key Lab Chem Biol, Minist Educ,Sch Pharmaceut Sci, Jinan 250012, Peoples R China.
来源:Mini reviews in medicinal chemistry
出版年:2014
卷:14
期:11
页码:884-895
DOI:10.2174/1389557514666141013141924
关键词:Anticancer;anticancer agents;ATP-competitive inhibitors;chemo- and radio-potentiation;DNA-dependent protein kinase (DNA-PK);DNA double-strand breaks (DSBs);DNA-PK inhibitors;DNA-PK catalytic subunit;PI3K;cytotoxicity;inhibitory activity;kinase selectivity
摘要:Repair of DNA double-strand breaks (DSBs) is critical for the maintenance of genome integrity, cell survival, and prevention tumorigenesis. Three pathways are responsible for the repair of DNA DSBs: homologous recombination (HR), single strand annealing (SSA) and non-homologous end joining (NHEJ). DNA-dependent Protein Kinase (DNA-PK), the key component of the NHEJ pathway, becomes an important target for cancer therapy. A large number of small molecules exhibit inhibitory activities against DNA-PK in an ATP-competitive manner. This paper reviews the recent developments of a diversity of small molecule DNA-PK inhibitors, with emphasis on their structural features, biological activities, and structure-activity relationships (SARs).
收录类别:SCOPUS;SCIE
WOS核心被引频次:1
Scopus被引频次:1
资源类型:期刊论文
原文链接:https://www.scopus.com/inward/record.uri?eid=2-s2.0-84911381436&doi=10.2174%2f1389557514666141013141924&partnerID=40&md5=df53e78bf30bca60b7e415323583f308
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